Development and characterization of monomeric N-end rule inhibitors through in vitro model substrates.

@article{Sriram2013DevelopmentAC,
  title={Development and characterization of monomeric N-end rule inhibitors through in vitro model substrates.},
  author={Shashi Sriram and Jeong Hoon Lee and Binh Khanh Mai and Yanxialei Jiang and Yongho Kim and Young Dong Yoo and Rajkumar Banerjee and S K Lee and Min Jae Lee},
  journal={Journal of medicinal chemistry},
  year={2013},
  volume={56 6},
  pages={2540-6}
}
In the N-end rule pathway, a set of N-terminal amino acids, called N-degrons, are recognized and ubiquitinated by the UBR proteins. Here we examined various N-end rule inhibitors to identify essential structural components of the system. Our study using in vitro biochemical assay indicated that the l-conformation and protonated α-amino group of the first residue were critical for N-degrons to properly interact with the UBR proteins. The monomeric molecules with minimum interacting motifs showed… CONTINUE READING

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